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对碳酸酐酶具有多价抑制作用的荧光二氧化硅纳米颗粒

Fluorescent Silica Nanoparticles with Multivalent Inhibitory Effects towards Carbonic Anhydrases.

作者信息

Touisni Nadia, Kanfar Nasreddine, Ulrich Sébastien, Dumy Pascal, Supuran Claudiu T, Mehdi Ahmad, Winum Jean-Yves

机构信息

Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS-ENSCM-Université de Montpellier, ENSCM, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex (France).

Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence (Italy).

出版信息

Chemistry. 2015 Jul 13;21(29):10306-9. doi: 10.1002/chem.201501037. Epub 2015 May 12.

DOI:10.1002/chem.201501037
PMID:25965260
Abstract

Multifunctional silica nanoparticles decorated with fluorescent and sulfonamide carbonic anhydrase (CA) inhibitors were prepared and investigated as multivalent enzyme inhibitors against the cytosolic isoforms hCA I and II and the transmembrane tumor-associated ones hCA IX and XII. Excellent inhibitory effects were observed with these nanoparticles, with KI values in the low nanomolar range (6.2-0.67 nM) against all tested isozymes. A significant multivalency effect was seen for the inhibition of the monomeric enzymes hCA I and II compared to the dimeric hCA IX and hCA XII isoforms, where no multivalent effect was observed, suggesting that the multivalent binding is occurring through enzyme clustering.

摘要

制备了用荧光和磺酰胺碳酸酐酶（CA）抑制剂修饰的多功能二氧化硅纳米颗粒，并将其作为针对胞质同工型hCA I和II以及跨膜肿瘤相关同工型hCA IX和XII的多价酶抑制剂进行了研究。这些纳米颗粒表现出优异的抑制效果，对所有测试同工酶的抑制常数（KI）值处于低纳摩尔范围（6.2 - 0.67 nM）。与二聚体hCA IX和hCA XII同工型相比，在抑制单体酶hCA I和II时观察到显著的多价效应，而在hCA IX和hCA XII同工型中未观察到多价效应，这表明多价结合是通过酶聚集发生的。

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